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Preparation and Characterization of Enrofloxacin Nanoparticles and its Pharmacokinetics in Domestic Emus (Dromaius novaehollandiae)

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Title Preparation and Characterization of Enrofloxacin Nanoparticles and its Pharmacokinetics in Domestic Emus (Dromaius novaehollandiae)
 
Creator Senthilkumar, P.
 
Contributor Arivuchelvan, A.
 
Description The study was conducted to formulate the enrofloxacin solid lipid nanoparticles
(SLN) with sustained release profile and improved pharmacological activity and evaluate the
pharmacokinetic behaviour of native and enrofloxacin SLN after different routes of
administration in emus. The SLN were prepared using tripalmitin as lipid carrier, tween 80
and span 80 as surfactants and poly vinyl alcohol (PVA) as a stabilizer by a hot
homogenization coupled with ultrasonication method. The influence of factors such as
concentration of lipid carrier, composition and concentration of surfactant on the particle
size were investigated to optimize the formulations. The optimized SLN formulations were
utilized to entrap 0.1% enrofloxacin and characterized for particle size, polydispersity index,
zeta potential (using dynamic light scattering), shape (using atomic force microscopy and
transmission electron microscopy), drug encapsulation efficiency (using by dialysis and
ultracentrifugation methods), and in vitro drug release (using by dialysis). The prepared
SLN were analyzed by FT-IR spectroscopy to confirm the cross-linking reaction between
drug, lipid and surfactants.
Pharmacokinetics of native enrofloxacin was studied after intravenous bolus, oral
bolus and in-water (pulse dosing) routes of administration at 10mg/kg in healthy emus aged
between 18 to 24 month and it was compared with disposition kinetics of enrofloxacin SLN.
Blood samples were collected at predetermined time intervals. Enrofloxacin and
ciprofloxacin in plasma were analyzed by high performance liquid chromatography (HPLC).
Plasma concentrations versus time were analysed by a noncompartmental analysis.
The results demonstrated that the particle size, polydispersivity index, zeta potential,
encapsulation efficiency and loading capacity of the SLN were 154.72± 6.11nm, 0.42±0.11,
-28.83±0.60mV, 59.66±3.22% and 6.13±0.32%, respectively. TEM and AFM images
showed spherical to circular particles with well defined periphery. In vitro drug release
exhibited biphasic pattern with an initial burst release of 18% within 2h followed by
sustained release over 96h. FT-IR study suggested that during the process of formulations,
lipid and surfactants have not reacted with the drug to give rise to reactant products and it
was only physical mixture.
For intravenous bolus, oral bolus and pulse dose of administration, elimination halflife
(t1/2β) was 4.364±0.179h, 4.125±0.361h and 4.066±0.295h, respectively; AUC0-∞ was
20.085±3.493μg.h/mL, 0.056±1.436μg.h/mL and 4.807±1.766μg.h/mL, respectively; mean
residence time (MRT) was 5.105±0.216h, 6.616±0.475h and 6.942±0.572h, respectively;
volume of distribution (Vdarea/F) was 3.921±1.005L/kg, 3.881±0.234L/kg and
4.177±0.275L/kg, respectively and total body clearance (CLB/F) was 0.629±0.164 L/h.kg,
0.646±0.052L/h.kg and 0.713±0.064L/h.kg , respectively. Mean absolute bioavailability for
enrofloxacin after oral bolus and pulse dose routes of administration was 79.941±7.147%
and 73.723±8.792%, respectively. In the present study, the plasma concentration of
metabolite ciprofloxacin was not consistent in emus
Comparison of the mean pharmacokinetic parameters between the routes of
administration of native enrofloxacin revealed significant (p
 
Date 2016-08-03T09:43:25Z
2016-08-03T09:43:25Z
2014
 
Type Thesis
 
Identifier http://krishikosh.egranth.ac.in/handle/1/70655
 
Language en
 
Format application/pdf
 
Publisher Tamil Nadu Veterinary and Animal Sciences University